1. PROTAC Protein Tyrosine Kinase/RTK Neuronal Signaling
  2. PROTACs Trk Receptor
  3. PROTAC NTRK1 degrader-1

PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors.
(Pink: NTRK1 ligand (HY-185545); Blue: Cereblon ligand (HY-W1115186); Black: linker).

For research use only. We do not sell to patients.

PROTAC NTRK1 degrader-1

PROTAC NTRK1 degrader-1 Chemical Structure

CAS No. : 2922274-35-7

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Description

PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors[1]. (Pink: NTRK1 ligand (HY-185545); Blue: Cereblon ligand (HY-W1115186); Black: linker).

In Vitro

NTRK degrader-1 (compound 5b) (6 h) degrades wild-type NTRK1, NTRK1G595R, NTRK1G667C, and NTRK1F598L in 293 T cells at 6 h, with the IP (inflection point) values of 0.2 nM, 1 nM, 2 nM, and 0.2 nM, respectively[1].
NTRK degrader-1 inhibits wild-type NTRK1, NTRK1G595R, NTRK1G667C, and NTRK1F598L with IC50 values of 4 nM, 2 nM, 5 nM and <0.5 nM, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics
Species Dose Route CL T1/2 Vss
Mice[1] 0.5 mg/kg i.v. 62 mL/mg/kg 1.6 h 3.1 L/kg
Molecular Weight

746.75

Formula

C38H35FN10O6

CAS No.
SMILES

O=C1NC(C=CC(C(NCC(N2CCN(C3=CC=C(NC4CCC(NC4=O)=O)C=C3)CC2)=O)=O)=C5)=C5OC(C=CC(F)=C6)=C6CNC7=NC8=C1C=NN8C=C7

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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PROTAC NTRK1 degrader-1
Cat. No.:
HY-181052
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